Alkylating agents Flashcards
Busulfan
AD VERSEEFFECT S
Severe myelosuppression (in almost all cases), pulmonary
fibrosis, hyperpigmentation
Busulfan
MECHANISM
Cross-links DNA
Nitrogen mustards
Cyclophosphamide,
ifosfamide
MECHANISM
Cross-link DNA
Require bioactivation by liver
Nitrogen mustards
Cyclophosphamide,
ifosfamide
AD VERSEEFFECT S
Myelosuppression, SIADH, Fanconi syndrome
(ifosfamide), hemorrhagic cystitis and bladder cancer
(prevent with mesna)
Nitrosoureas
Carmustine, lomustine
MECHAN ISM
Cross-link DNA Require bioactivation by liver
Cross blood-brain barrier
Nitrosoureas
Carmustine, lomustine
AD VERSEEFFECT S
CNS toxicity (convulsions,
dizziness, ataxia)
Procarbazine
mechanism
Mechanism unknown
Weak MAO inhibitor
procarbazine
adverseffect
Myelosuppression, pulmonary
toxicity, leukemia, disulfiramlike reaction
Temozolomide
mechanism
DNA methylation
Temozolomide
adverseffect
Myelosuppression
Platinum compounds
Cisplatin, carboplatin, oxaliplatin.
MECHANISM
Cross-link DNA. Cell cycle nonspecific.
Platinum compounds
Cisplatin, carboplatin, oxaliplatin.
AD VERSE EFFECT S
Nephrotoxicity (eg, Fanconi syndrome; prevent with amifostine), peripheral neuropathy, ototoxicity.
Taxanes
Docetaxel, paclitaxel
mechanism
Hyperstabilize polymerized microtubules → prevent mitotic spindle breakdown
Taxanes
Docetaxel, paclitaxel
AD VERSEEFFECT S
Myelosuppression, neuropathy,
hypersensitivity
Vinca alkaloids
Vincristine, vinblastine
mechanism
Bind β-tubulin and inhibit
its polymerization into
microtubules → prevent
mitotic spindle formation